Rupatadine

Identification

Name

Rupatadine

Accession Number

DB11614

Type

Small Molecule

Groups

Approved

Description

Rupatadine is a dual histamine H1 receptor and platelet activating factor receptor antagonist that is used for symptomatic relief in seasonal and perennial rhinitis as well as chronic spontaneous urticaria. It was approved for marketing in Canada under the tradename Rupall and comes in tablet formulation for adult use and liquid formulation for pediatric use.

Pharmacology

Indication

For the symptomatic relief of nasal and non-nasal symptoms of seasonal allergic rhinitis and perennial allergic rhinitis in patients 2 years of age and older [Label]. Also used for the symptomatic relief of chronic spontaneous urticaria in patients 2 years of age and older.

Rupatadine is an anti allergenic and acts to reduce allergic symptoms like urticaria, rhinorrhea, sneezing and itching [Label].

Mechanism of action

Rupatadine is a dual histamine H1 receptor and platelet activating (PAF) receptor antagonist [1][Label]. During allergic response mast cells undergo degranulation, releasing histamine and other substances [2]. Histamine acts on H1 receptors to produce symptoms of nasal blockage, rhinorhea, itching, and swelling. PAF is produced from phospholipids cleaved by phospholipase A2. It acts to produce vascular leakage which contributes to rhinorhea and nasal blockage. By blocking both the H1 receptor and PAF receptor, rupatidine prevents these mediators from exerting their effects and so reduces the severity of allergic symptoms.

Rupatadine is metabolized by oxidation mediated primarily by CYP3A4 [Label]. CYP2C9, CYP2C19, and CYP2D6 are also involved to a lesser extent. The metabolites desloratidine and hydroxylated forms of desloratidine retain some activity as H1 receptor antagonists.

Route of elimination

Not Available

Half life

The half life of elimination is 15.9 h in children 2-5 years old, 12.3 h in children 6-11 years old, 5.9 h in adults, and 8.7 h in geriatric patients [Label].

Clearance

Systemic clearance is 1556.2 L/h in young adults and 798.2 L/h in geriatric patients [Label].

Taxonomy

Description

This compound belongs to the class of organic compounds known as benzocycloheptapyridines. These are aromatic compounds containing a benzene ring and a pyridine ring fused to a seven membered carbocycle.